Publication number: 20180282328
Abstract: Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
Type:
Application
Filed:
March 30, 2018
Publication date:
October 4, 2018
Applicant:
Genentech, Inc.
Inventors:
Bryan Chan, Blake Daniels, Joy Drobnick, Lewis Gazzard, Timothy Heffron, Malcolm Huestis, Jun Liang, Sushant Malhotra, Rohan Mendonca, Naomi Rajapaksa, Michael Siu, Craig Stivala, John Tellis, Weiru Wang, BinQing Wei, Aihe Zhou, Matthew W. Cartwright, Emanuela Gancia, Graham Jones, Michael Lainchbury, Andrew Madin, Eileen Seward, David Favor, Kin Chiu Fong, Andrew Good, Yonghan Hu, Baihua Hu, Aijun Lu
Publication number: 20180125997
Abstract: Conjugate compounds of formula (A): wherein: R2 is where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester; or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 43; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, wher
Type:
Application
Filed:
October 17, 2017
Publication date:
May 10, 2018
Inventors:
Philip Wilson HOWARD, John A. FLYGARE, Thomas PILLOW, Binqing WEI
Patent number: 9821074
Abstract: Conjugate compounds of formula (A): wherein: R2 is ?where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
November 21, 2017
Assignees:
Genentech, Inc., MedImmue Limited
Inventors:
Philip Wilson Howard, John A. Flygare, Thomas Pillow, Binqing Wei